E-cigarette or vaping fluid

ABSTRACT

Improved vaping fluids for energy boos, relaxation, appetite and other functions contain active ingredients combined with cyclodextrin to enhance absorption and avoid irritation. Active ingredients include caffeine, theophylline, yerba mate and valerian as well as taurine, carnitine and L-tryptophan. The active ingredients are combined with an aqueous solution of hydrophilic solvents (such as glycerin or propylene glycol) as well as traces of scents or flavors.

CROSS-REFERENCE TO PRIOR APPLICATIONS

This application is based on and claims the priority and benefit of U.S.Provisional Patent Application No. 62/102,894 which was filed on 13 Jan.2015.

U.S. GOVERNMENT SUPPORT

Not applicable.

BACKGROUND OF THE INVENTION

1. Area of the Art

The current invention is in the area of e-cigarettes and “vaping” andconcerns an improved non-nicotine fluid for e-cigarette devices.

2. Description of the Invention

Smoking has a long history in human cultures. When plant materials areburned various organic chemicals that are constituents of the plantvaporize and attach themselves to the smoke particles. At the same timeheat and combustion break down constituent organic chemicals and producenew chemicals all of which are present in the vapor state and/or attachthemselves to the smoke particles. When the smoke is inhaled, theparticles come into contact with the surface of lung cells and thechemicals absorbed to the particles transfer to the lung cells andeventually are transferred into the circulatory system. Because of theextremely large surface area of the lung, smoking is an extremelyeffective route for administering active compounds. Because plantscontain a wide variety of secondary products inhaling the smoke deliversthese products to the human body. The physiological results can bestimulation, depression or even hallucination depending on what type ofplant is burned to produce the smoke.

Of course, the active molecules delivered by the smoke can be highlyaddictive as in the case of nicotine in tobacco smoke. Probably becauseof its addictive nature tobacco has become the primary plant materialthat is smoke worldwide—to the point that “smoking” has becomeessentially synonymous with “tobacco smoking.” Whereas tobacco smokingwas once considered to be a benign or even healthful pastime, it is nowconsidered to be a health hazard. Over the last fifty years it has beenshown that tobacco smoking is major cause of lung as well as othercancers in smokers as well as those exposed to “second hand” smoke. Inaddition, there is a correlation between smoking tobacco and heart aswell as vascular disease.

It is true that because of the wide range of natural chemicals (“naturalproducts”) in plants, smoke from burning many different plants shows atleast some carcinogenic properties. However, for whatever reason itappears as if tobacco smoke may be more carcinogenic than other types ofsmoke. In addition, it also appears as if exposure to tobacco smokeresults in more vascular damage than other smoke exposure. This may bebecause there are insufficient data on long term exposure to other typesof smoke. Or perhaps chronic exposure to constituents of tobacco smokeresults in vascular damage. In any case, there is a worldwide effort toreduce or eliminate tobacco smoking. Today smoking is prohibited onairlines, in most restaurants and buildings as well as a variety ofother locales. Because nicotine is addictive, there is a major industrythat attempts to help smokers stop smoking.

“Electronic cigarettes” (e-cigarettes) have been developed as a saferalternative to smoking tobacco. In an e-cigarette a mechanism reduces aliquid (“e-cigarette fluid,” “e-fluid” or “vaping fluid”) into asmoke-like mixture of air and tiny droplets (an aerosol) which materialis then inhaled. Any active constituents in the vaping fluid are thenabsorbed by the lungs like real smoke. Because e-cigarettes do notproduce smoke, other terms have been developed to describe using thedevices. One such term that is gaining popularity is “vaping.” Thus, onedoes not smoke an e-cigarette—one “vapes” it. E-cigarettes are thoughtto be safer than smoking tobacco because nothing is actually burned inan e-cigarette. The most common type of e-cigarette has a heatingelement which vaporizes the e-fluid to create an aerosol. Less commonlythere is mechanical production of the aerosol. For example, some devicesuse a piezoelectric diaphragm which vibrates at ultrasonic speeds todirectly form an aerosol from the e-fluid rather like a cool-misthumidifier.

Most e-fluids contain nicotine (approximately 0.04M-0.12M) so thatvaping an e-cigarette can act as a substitute for smoking tobacco bydelivering nicotine to the user. There is considerable use of suchnicotine e-cigarettes as smoking cessation devices. The idea is that theusers transition to the e-cigarettes and then use e-fluids withdiminishing levels of nicotine until the user's nicotine addiction isovercome. However, many users alternate between “real” cigarettes ande-cigarettes so the usefulness of vaping e-cigarettes as an aid tosmoking cessation is somewhat questionable. Certainly, the e-cigaretteavoids the dangers of secondhand tobacco smoke.

There has been considerable development of e-fluid formulations withvarious flavors and scent ingredients being added to enhance the user'senjoyment. In addition, e-fluids without any nicotine have beenmarketed. The idea being that the user will sufficiently enjoy vaping sothat nicotine becomes unnecessary. However, if the goal is to replaceaddictive nicotine, it is probably necessary to provide some otheractive component so that the user gets some sort of physiological resultfrom the vaping process.

There is a very long history of humans ingesting various plant productsfor their physiological effects. Some plant products are intoxicating oreven hallucinogenic. Generally, such materials are subject to strictlegal controls. Other plant products are stimulants many of which arelegal and widely used such as the methylxanthines: caffeine (coffee),theobromine (chocolate) and theophylline (tea). These agents improveenergy and feeling of well-being. These stimulants are considered safeand many people enjoy their effects. The present inventor has consideredsubstituting them for nicotine in e-fluid. It is believed thatsecondhand “smoke” from e-cigarettes containing methylxanthinederivatives would be free of the health concerns that attend secondhande-cigarette nicotine “smoke.” There is a long history of inhaling strongpreparations of theophylline and other methylxanthine derivatives as abronchial dilator for the treatment of asthma and other obstructive lungconditions. Inhalation of these agents has not been associated withsignificant health problems. Therefore, use of much lower concentrationsof methylxanthine derivatives in e-fluids is unlikely to have anynegative health consequences. However, when inhaled, these agents willbe systemically absorbed with general stimulant effects similar toconsuming methylxanthine containing beverages. This will impart thephysiological result to enhance the desirability of vaping.

SUMMARY OF THE INVENTION

The inventors have discovered that improved vaping fluids can beobtained by combining a variety of active ingredients with thehydrophilic solvents typical of such fluids. The active ingredients arechosen depending on the desired effects of using the fluid. For example,methylzanthines such as caffeine can be used to provide an energy boostproduct. Energy boost formulae can also contain taurine, cyanocobalamin,carnitine, guarana, and ginseng. Relaxation/sleep formulae can includechamomile, valerian, kava and other active ingredients. Appetitesuppressant formulae can contain hoodia, yerba mate, caralluma andlecithin. Besides active ingredients a variety of scents/flavors andcolors can also be included. It is preferred to used natural plantextracts to impart colors. Cyclodextrin is included to enhanceabsorption of the active ingredients as well as to limit any tendency ofthe inhaled aerosol to cause irritation. Detailed Description of theInvention

The following description is provided to enable any person skilled inthe art to make and use the invention and sets forth the best modescontemplated by the inventor of carrying out his invention. Variousmodifications, however, will remain readily apparent to those skilled inthe art, since the general principles of the present invention have beendefined herein specifically to provide improved non-nicotine fluids forvaping.

Generally, e-fluids contain water and one or more hydrophilic solventsuch as glycerol, propylene glycol and/or polyethylene glycol. Thehydrophilic solvent is important for the production of aerosols by aheat source. When a water solution of these solvents contacts a heatsource, the water rapidly vaporizes leaving behind an aerosol ofhydrophilic solvent particles which contain the other ingredients thatwere dissolved in the original e-fluid and/or the other ingredients arepresent as tiny particles. The “other ingredients” (besides “active”ingredients such as nicotine, in traditional e-fluid, or methylxanthineor other active ingredients in the alternative e-fluid disclosed here)include flavors, scents and additives intended to enhance the efficacyof the other ingredients. To be effective the ingredients must becarried into the user's lungs. This generally occurs because theingredients are bound to or dissolved in the aerosol particles. However,the aerosol particles may not always be of optimum size so that they arefiltered out by lung structures before there is a chance for the activeingredients to be properly absorbed. In other cases the aerosolparticles are somewhat irritating to the user's throat and othertissues.

The problem with the aerosol particles not being efficiently absorbedcan be dealt with by increasing the concentration of the activeingredients. However, this may also increase the ability of theparticles to cause irritation. Where the active ingredient is nicotine,it can be dangerous to increase the nicotine concentration too muchsince nicotine is extremely toxic. What is needed is a method to enhancethe effectiveness of active ingredients while at the same time reducingany propensity for irritation. The present inventor has found thatcertain polysaccharides can serve this function. Addition ofcyclodextrin to e-fluid enhances the absorbability of active ingredientswhile suppressing any irritating tendency of the aerosol. Cyclodextrinis a cyclic polysaccharide made of a 1, 4 linked glucose units. Thereare three common types: a cyclodextrin (6 glucose units), cyclodextrin(7 glucose units) and γ cyclodextrin (8 glucose units). It is known thatcyclodextrins are useful for sequestering hydrophobic molecules and forforming droplets in a nebulizer. Until now it was not appreciated thatcyclodextrins also promote aerosol formation with the heating elementsof common e-cigarettes (as well as with the spray jets of nebulizers).More importantly, the addition of sufficient cyclodextrin to e-fluidenhances the absorption and bioavailability of any active ingredientswhile at the same time reducing any tendency towards irritation causedby the aerosol.

In solution the cyclodextrin molecules form a somewhat conicalstructure—that is, a hollow cylinder having a smaller opening at one endthan the other. The cyclodextrin molecule in solution has an interiorthat is more hydrophobic than its exterior (i.e., the exterior isrelatively hydrophilic). For the cyclodextrin to operate in the currentinvention, the molecule to be sequestered must be at least partiallyhydrophobic and of dimensions to fit within the cyclodextrin ring.Active ingredients such as methylxanthines and nicotine are of the rightsize for sequestration and are essentially hydrophobic at physiologicaland acid pHs. The choice of cyclodextrin is affected by the activeingredient as well as the other ingredients in the e-fluid formula. Bothα and γ cyclodextrin have a water solubility that is approximately anorder of magnitude higher than that of β cyclodextrin. Therefore, if itis desired to use a relatively high level of active ingredient, a and γcyclodextrin are preferred. Otherwise, β cyclodextrin operatesadequately.

Active Ingredients

For an “Energy Boost” formulation a methylxanthine alkaloid such ascaffeine is combined with taurine which has beneficial biological aswell as surfactant properties. As already explained methylxanthinealkaloids improve energy and provide a feeling of well-being. Taurine isa natural amino acid derivative that has an anti-anxiety effect as wellas many health benefits. In addition, taurine has surfactant propertiesand aids in the dispersion of insoluble ingredients. Caffeine iseffective in e-fluids of 0.01M to 0.15M. Much below this concentrationrange, there is little discernible effect whereas at much higherconcentrations, the caffeine effect can be excessive. Currently, aconcentration of 0.05M is preferred. Taurine has a wide effective rangeof at least 0.01M to 0.1M; currently 0.015M is preferred. To theseactive ingredients can be added cyanocobalamin (vitamin B12). This watersoluble vitamin is important for many cellular functions and seems topotentiate the effects of caffeine and taurine. The cyanocobalamin has ared-magenta color and can be used as the sole coloring agent or othercolors may be added as desired. This has been tested at concentrationsbetween 0.01% and 0.1%; currently 0.083% (weight by volume) ispreferred. Other common methylxanthines such as theophylline ortheobromine can be substituted or used in conjunction with caffeine.

Other “Energy Boost” ingredients can be used either alone or inconjunction with the methylxanthines. For example, green tea extractscan be employed not only as a source of caffeine and theophylline butalso for beneficial antioxidants (and to impart a flavor). Extracts ofguarana (Paullinia cupana) can be used to supply caffeine as well asother beneficial natural ingredients. Extracts of Ginkgo biloba can beused to supply antioxidants Extracts of ginseng (Panax species) are alsoeffective when combined with cyclodextrins. Finally, carnitine iseffective in energy formulae. These ingredients are generally used atconcentration of about 0.5% by weight or less.

Caffeine, other methylxanthines and taurine can be stabilized as metalcomplexes (zinc, magnesium and/or sodium) and/or cyclodextrin complexes.Metal complexes are formed by adding a molar excess of a water solublesalt of the desired metal. Cyclodextrin complexes form best with a molarexcess of cyclodextrin. It has been found that a 2-3 fold molar excessworks well although cyclodextrin is effective in the range of 0.5 to 5.0molar ratio of cyclodextrin to active ingredient. Cyclodextrin is usedpreferable but can be used with the metal complex as well. That is, therequired concentration of both metal and cyclodextrin can be used.

Besides Energy formulae, “Relaxation/sleep” formulae are also useful. Inthese formulae ingredients such as extracts of chamomile (Matricariachamomilla and/or Chamaemelum nobile), extracts of kava (Pipermethysticum), extracts of valerian (Valeriana officinalis), L-tryptophanand/or melatonin are used in place of the “energy” ingredients. Againthese ingredients are used in the 0.5% by weight or lower concentrationrange.

Finally, it is also possible to use safe appetite suppressants in placeof the energy ingredients to yield a “weight loss” formula. Variousplant extracts are useful—in particular extracts of yerba mate (Ilexparaguariensis), extracts of Hoodia gordonii and extracts of Caraflumafimbriata. In addition, certain compounds such as chromium chelate andlecithin are useful in these formulae. The chromium is used at a fewparts per million (ppm) while the other ingredients are used up to 0.5%by weight.

Vehicle and Inactive Ingredients

The main vehicle is an approximately 50% aqueous solution of highboiling point hydrophilic solvent. It is not essential that the fluid beprecisely 50% water. Typically either glycerol and/or propylene glycolare used as hydrophilic solvents. This translates to a 5.4M glycerol ora 6.6M propylene glycol solution. Tests suggest that a solution being atleast about 2M of either of these solvents (or a combination thereof) isadequate. Using excess hydrophilic solvent increases both the cost andviscosity of the product. The hydrophilic solvents increase thesolubility of the active ingredients and act as particle formers whenthe e-cigarette mechanism boils away much of the water. Without thesesolvents aerosol formation would be much less efficient.

Besides the vehicle, the inactive ingredients include a variety offlavors and/or scents. Actually, these additives are primarily scentsbecause the human sense of taste is primarily limited to sweet, salty,sour, bitter and umami. What we perceive of as “orange” flavor or tasteis actually orange scent combined with a taste of sweet and sour. Theglycerol and propylene glycol components of the vehicle have an actualsweet taste that can be detected by most users. Depending on the pH ofthe vehicle there may also be a slight sour (low pH) taste. If activeingredients such as caffeine or nicotine are present at sufficientlyhigh concentrations, there may also be an actual discernible bittertaste. Useful scents are practically unlimited. Traditionally, mentholand mint-related scents were used in tobacco cigarettes. Therefore,mint-related scents are useful in e-fluid. In addition, fruit flavors(i.e., orange and banana) are popular as are more floral or “perfumed”scents such as vanilla. Currently, the preferred “flavors” are greenapple, vanilla cupcake, blueberry, and mango. However, various herbal,musky and other scents may also be appropriate. Generally, these areused at very low concentrations. Generally, under 0.1% by volume. Manyof the plant extracts mentioned above also provide a uniqueflavor/scent.

Sample e-fluid formulae are given in the following tables.

Energy Boost (100 ml)

Ingredient Concentration Caffeine 0.05M Taurine 0.015M MagnesiumChloride 0.06M Cyanocobalamin 0.083% (weight by volume) Cyclodextrin0.2M Scent/Flavor trace Vehicle To make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

Focus Boost (100 ml)

Ingredient Concentration Ginkgo biloba extract 0.25% (volume by volume)Carnitine 0.1% (weight by volume)M Magnesium Chloride 0.06M Cyclodextrin0.2M Scent/Flavor trace Vehicle To make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

Focus Boost II (100 ml)

Ingredient Concentration Taurine 0.015M Sodium Chloride 0.06MCyanocobalamin 0.083% (weight by volume) Cyclodextrin 0.05M Scent/Flavortrace Vehicle To make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

Sleep (100 ml)

Ingredient Concentration Valerian extract 0.5% (volume by volume)Chamomile extract 0.25% (volume by volume Sodium Chloride 0.06MCyclodextrin 0.05M Scent/Flavor trace Vehicle To make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

Appetite suppressant (100 ml)

Ingredient Concentration Yerba mate extract 0.5% (volume by volume)Lecithin 0.5% (weight by volume) Cyclodextrin 0.05M Scent/Flavor traceVehicle To make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

Flavor only (100 ml)

Ingredient Concentration Cyclodextrin 0.01M Scent/Flavor trace VehicleTo make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

Enhanced Traditional (nicotine containing) (100 ml)

Ingredient Concentration Nicotine 0.08M Taurine 0.015M Sodium Chloride0.015M Cyanocobalamin 0.083% (weight by volume) Cyclodextrin 0.2MScent/Flavor trace Vehicle To make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

Improved Traditional (nicotine containing) (100 ml)

Ingredient Concentration Nicotine 0.08M Cyclodextrin 0.1M Scent/Flavortrace Vehicle To make 100 ml

The ingredients are mixed, the pH adjusted to 6.5 and heated to 60° C.to ensure that the scent/flavor is properly dispersed.

The following claims are thus to be understood to include what isspecifically illustrated and described above, what is conceptuallyequivalent, what can be obviously substituted and also what essentiallyincorporates the essential idea of the invention. Those skilled in theart will appreciate that various adaptations and modifications of thejust-described preferred embodiment can be configured without departingfrom the scope of the invention. The illustrated embodiment has been setforth only for the purposes of example and that should not be taken aslimiting the invention. Therefore, it is to be understood that, withinthe scope of the appended claims, the invention may be practiced otherthan as specifically described herein.

What is claimed is:
 1. An e-fluid for use in an e-cigarette or similardevice comprising: caffeine at a concentration of between about 0.01M toabout 0.15M; cyclodextrin at a concentration having a molar ratio withthe caffeine concentration of 0.5 to 5.0; and an aqueous solution ofhydrophilic solvent being between about 2M and 10M hydrophilic solvent.2. The e-fluid of claim 1 wherein the hydrophilic solvent is selectedfrom the group consisting of glycerol and propylene glycol.
 3. Thee-fluid of claim 1 further comprising carnitine at a concentration ofabout 0.01% and about 0.5% volume by volume.
 4. The e-fluid of claim 1further comprising taurine at a concentration of between about 0.01M andabout 0.1M.
 5. The e-fluid of claim 1 further comprising cyanocobalaminat a concentration of between about 0.01% weight by volume and 0.1%weight by volume.
 6. An e-fluid for use in an e-cigarette or similardevice comprising: valerian extract at a concentration of between about0.01% and about 0.5% volume by volume; cyclodextrin at a concentrationhaving a molar ratio with the valerian extract concentration of 0.5 to5.0; and an aqueous solution of hydrophilic solvent being between about2M and 10M hydrophilic solvent.
 7. The e-fluid of claim 6 wherein thehydrophilic solvent is selected from the group consisting of glyceroland propylene glycol.
 8. The e-fluid of claim 6 further comprisingL-tryptophan at a concentration of about 0.01% and about 0.5% weight byvolume.
 9. The e-fluid of claim 6 further comprising extract ofchamomile at a concentration of about 0.01% and about 0.5% volume byvolume.
 10. The e-fluid of claim 6 further comprising cyanocobalamin ata concentration of between about 0.01% weight by volume and 0.1% weightby volume.
 11. An e-fluid for use in an e-cigarette or similar devicecomprising: nicotine at a concentration of between about 0.01 M to about0.2M; cyclodextrin at a concentration having a molar ratio with thenicotine concentration of 0.5 to 5.0; and an aqueous solution ofhydrophilic solvent being between about 2M and 10M hydrophilic solvent.12. The e-fluid of claim 11 wherein the hydrophilic solvent is selectedfrom the group consisting of glycerol and propylene glycol.
 13. Thee-fluid of claim 11 further comprising taurine at a concentration ofbetween about 0.01M to about 0.1M.
 14. The e-fluid of claim 11 furthercomprising cyanocobalamin at a concentration of between about 0.01%weight by volume and 0.1% weight by volume.